Dissolution Efficacy Research Articles

Seafloor alkalinity enhancement as a carbon dioxide removal strategy in the Baltic Sea

Carbon dioxide removal from the atmosphere and storage over long times scales in terrestrial and marine reservoirs is urgently needed to limit global warming and for sustainable management of the global carbon cycle. Ocean alkalinity enhancement by the artificial addition of carbonate minerals to the seafloor has been proposed as a method to sequester atmospheric CO2 and store it in the ocean as dissolved bicarbonate. Here, a reaction-transport model is used to scrutinize the efficacy of calcite addition and dissolution at a well-studied site in the southwestern Baltic Sea – a brackish coastal water body in northern Europe. We find that most calcite is simply buried without dissolution under moderate addition rates. Applying the model to other sites in the Baltic Sea suggests that dissolution rates and efficiencies are higher in areas with low salinity and undersaturated bottom waters. A simple box model predicts a tentative net CO2 uptake rate from the atmosphere of 3.2 megatonnes of carbon dioxide per year for the wider Baltic Sea after continually adding calcite to muddy sediments for 10 years. More robust estimates now require validation by field studies.

Compatibility of Dual Rinse 1-Hydroxyethane-1,1-Diphosphonic Acid with Sodium Hypochlorite Solutions Containing Proprietary Additives

IntroductionA salt of 1-hydroxyethylidene-1,1-diphosphonic acid (HEDP) was commercialized some years ago. This so-called Dual Rinse (DR) HEDP has been tested for its combined actions and interactions with pure sodium hypochlorite (NaOCl) solutions. The aim of this study was to assess DR interactions with NaOCl solutions containing proprietary additives. MethodsDesignated endodontic NaOCl solutions that come at 2 different strengths (2% and 5.25%), and without or with additives (Chloraxid and Chloraxid Extra, respectively) were tested. Some of their key chemical and physical properties were determined in the presence or absence of HEDP (9%) in the solution. In addition, soft tissue dissolution efficacy of test and control solutions was assessed in extracted teeth (n = 10 per group, 90 teeth in total). ResultsThe NaOCl content in the 2% Chloraxid solutions was slightly above, that in the 5.25% solutions below the labeled concentration. The additives in the Chloraxid Extra solutions neither altered their surface tension nor their viscosity. The addition of HEDP to any of the tested NaOCl solutions reduced their pH, and increased their surface tension and viscosity. HEDP-induced available chlorine loss over the first hour was similar between all NaOCl solutions. Soft tissue dissolution in the root canals was affected by NaOCl concentration, but neither by any proprietary NaOCl additive in the Chloraxid solutions, nor the addition of DR HEDP. ConclusionsProprietary additives had no influence on any of the tested parameters, including surface tension of the "Extra" solutions. The increased viscosity of combined NaOCl/HEDP solutions deserves further attention.

Effect of direct oral anticoagulant therapy on pulmonary artery clot dissolution in intermediate high-risk pulmonary thromboembolism

BackgroundDirect oral anticoagulants are the established drugs for treating pulmonary thromboembolism. The advantage of direct oral anticoagulants over conventional therapy for clot lysis and right ventricular unloading in the acute phase remains unclear. This study aimed to evaluate the effect of acute treatment with direct oral anticoagulants on clot dissolution and right ventricular unloading in intermediate high-risk pulmonary thromboembolism.MethodsThirty patients with intermediate high-risk pulmonary thromboembolism admitted between November 2012 and December 2018 were included; 21 and 9 were treated with direct oral anticoagulants and conventional therapy, respectively. We compared the efficacy of clot dissolution and right ventricular unloading for intermediate high-risk pulmonary thromboembolism between direct oral anticoagulant and conventional therapy in the acute phase. Efficacy was assessed by computed tomography obstruction index, right/left ventricular ratio, and brain natriuretic peptide levels between baseline and at discharge.ResultsComputed tomography obstruction index, right ventricular/left ventricular ratio, and brain natriuretic peptide levels were significantly lower at discharge than at admission in both groups. The rate of improvement in computed tomography obstruction index was significantly higher in the direct oral anticoagulant therapy group than in the conventional therapy group (64 ± 15% vs. 47 ± 16%; p = 0.01). There were no significant differences in the rate of improvement in right ventricular/ left ventricular ratio and brain natriuretic peptide levels between the two groups.ConclusionsCompared with conventional therapy, direct oral anticoagulants significantly reduced pulmonary artery clot burden conventional therapy in the acute treatment of intermediate high-risk pulmonary thromboembolism.

Assessing the efficacy of various irrigation solutions in dissolving organic tissue

For successful root canal treatment, adequate chemomechanical instrumentation to eliminate microorganisms and pulp tissue is crucial. This study aims to assess the organic tissue dissolving activity of various irrigation solutions on bovine tooth pulp tissue. 40 extracted bovine mandibular anterior teeth (n = 10) were used for the study. Bovine pulp pieces (25 ± 5 mg) were placed in 1.5 ml Eppendorf tubes. Each tooth pulp sample was then covered with 1.5 ml of different irrigation solutions, dividing them into four groups: Group 1 with freshly prepared 5% Boric acid, Group 2 with 5% NaOCl, Group 3 with Irritrol, and Group 4 with Saline. Samples were left at room temperature for 30 min, then dried and reweighed. The efficacy of tissue dissolution ranked from highest to lowest was found to be NaOCl, Boric Acid, Irritrol, and saline (p < 0.05). It was observed that the decrease in the NaOCl group was greater than the decrease in the Irritrol and saline groups, and the decrease in the Boric acid group was significantly greater than the decrease in the saline group (p < 0.05). It also emphasizes the need for future studies to further investigate the effects of Irritrol and Boric Acid on tissue dissolution.

New Excipient For Oral Drug Delivery: CNC Derived From Sugarcane Bagasse-Derived Microcrystalline Cellulose.

Nanocrystalline cellulose (CNC) has emerged as a subject of researcher's interest because of its diverse attributes encompassing biocompatibility, sustainability, a high aspect ratio, and an abundance of -OH groups suitable for modifications. Sugarcane bagasse microcrystalline cellulose (SCBMCC) was used as the raw material for the preparation of CNC due to its pure cellulose content, which is mildly compromised by the pectin, hemicellulose, lignin, and other lignocellulosic components. In the present work, CNC was extracted from SCBMCC and used as a disintegrant. The classic hydrolysis technique was used for the preparation of CNC. Hydrolytic conditions were optimized using the response surface methodology (RSM). The optimized batch of CNC was characterized using techniques such as field-emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. Notably, CNC prepared under a hydrolysis time of 90 min exhibited the highest crystallinity of 69.9%. The average particle size and zeta potential were found to be 145 nm and -34.4 mV, respectively. Thermal analysis suggested that an intermediate hydrolysis time resulted in CNC with enhanced thermal stability, showcasing its potential for pharmaceutical applications. Diclofenac potassium was used as the model drug to evaluate the disintegrant properties of CNC as an excipient. Tablets were prepared using the direct compression method. SCBMCC and CNC were used as disintegrants and were compared with the commercial product. The disintegration times (DTs) attained for the tablets prepared using CNC and SCBMCC are 219 and 339.83 s, respectively. The dissolution study of CNC showed a dissolution efficacy (DE%) of 66 and a mean dissolution time (MDT) of 12. The research findings showed that tablets prepared using CNC as disintegrants exhibited the fastest disintegration compared to other formulations.

Drug-Polymer Nanodroplet Formation and Morphology Drive Solubility Enhancement of GDC-0810.

Nanodroplet formation is important to achieve supersaturation of active pharmaceutical ingredients (APIs) in an amorphous solid dispersion. The aim of the current study was to explore how polymer composition, architecture, molar mass, and surfactant concentration affect polymer-drug nanodroplet morphology with the breast cancer API, GDC-0810. The impact of nanodroplet size and morphology on dissolution efficacy and drug loading capacity was explored using polarized light microscopy, dynamic light scattering, and cryogenic transmission electron microscopy. Poly(N-isopropylacrylamide-stat-N,N-dimethylacrylamide) (PND) was synthesized as two linear derivatives and two bottlebrush derivatives with carboxylated or PEGylated end-groups. Hydroxypropyl methylcellulose acetate succinate grade MF (HPMCAS-MF) and poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA) were included as commercial polymer controls. We report the first copolymerization synthesis of a PVPVA bottlebrush copolymer, which was the highest performing excipient in this study, maintaining 688 μg/mL GDC-0810 concentration at 60 wt % drug loading. This is likely due to strong polymer-drug noncovalent interactions and the compaction of GDC-0810 along the PVPVA bottlebrush backbone. Overall, it was observed that the most effective formulations had a hydrodynamic radius less than 25 nm with tightly compacted nanodroplet morphologies.

A Comparative Evaluation of Pulp Tissue Dissolving Ability of Three Different Pulp Dissolving Agents With 5.25% Sodium Hypochlorite: An In-Vitro Study

Introduction: The dissolution of pulp tissue is an essential aspect of root canal treatment, as it aids in the removal of necrotic or infected tissue from the root canal, thereby reducing the microbial load. Aim: This in-vitro study aimed to compare the pulp tissue dissolving ability of three different pulp-dissolving agents with a 5.25% sodium hypochlorite (NaOCl) solution. Materials and Methods: 128 intact, non-carious extracted human single-rooted premolar teeth were selected and sectioned to harvest intact pulp tissue. Pulp tissue samples were randomly divided into four experimental groups (n=32) based on the pulp dissolving agent used: Group I (5.25% NaOCl solution), Group (5% Calcium hypochlorite solution), Group III (5.25% NaOCl gel) and Group IV (8% Papain gel). The initial weight of each sample was recorded and samples were exposed to specific pulp-dissolving agents for specified time intervals. The time required for complete dissolution of the pulp tissue was recorded for all samples till 120 mins. Results: The study analyzed the mean weight of pulp tissue in various groups, including Group I, Group II, Group III, and Group IV. After 30 minutes, complete dissolution of pulp tissue was evident in Group I, while Group II showed 0.0058 grams of remaining tissue after 30 minutes, 0.0040 grams after 60 minutes, and 0.0022 grams after 120 minutes. Group III showed 0.0072 grams of remaining tissue after 30 minutes, and Group IV showed 0.0075 grams of remaining tissue after 30 minutes, 60 minutes, 90 minutes, and 120 minutes. Conclusion: 5.25% NaOCl has the highest pulp tissue dissolution efficacy compared to other dissolving agents. Further clinical studies are warranted to validate these findings and assess the feasibility of these agents in clinical practice.

Abstract 10 — Enhancing Dissolution Efficiency of Ketoprofen, A Rheumatoid Arthritis Pain Management Drug, through Solid Dispersion Formulation

Background Ketoprofen (KPN) is commonly prescribed drug to alleviate pain related with rheumatoid arthritis (RA). However, KETO belongs to the BCS class-II category, characterized by poor water solubility, resulting in less dissolution capability leading to limited systemic absorption. Purpose of this study was to increase aqueous solubility as well as rate of dissolution of KPN using solid-dispersion technique. Methods Two different hydrophilic carriers, D-mannitol and polyvinylpyrrolidone K30 (PVP K30) and, were utilized, in varying ratios with the drug, to formulate solid dispersions. Kneading and solvent evaporation techniques were employed for preparing KPN solid dispersions with PVP K30, while kneading and melting methods were utilized for solid dispersions containing D-mannitol. The liquid state of the formulations was characterized through phase-solubility studies, while Scanning Electron Microscopy (SEM), Fourier Transform Infrared (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC) and X-ray diffraction (XRD) analysis were performed to examine the solid state. Results Both carriers demonstrated a favorable impact on the aqueous solubility of KPN. Solid state examination of D-mannitol solid dispersions revealed that KPN existed as fine particles, while it was entrapped within the polymer matrix in solid dispersions with PVP K30. Compared to poor rate of dissolution of pure drug KPN, the drug dispersions in both carriers showed a significantly improved dissolution rate. Improvement of dissolution rate can be ascribed to enhanced wetting behavior and dispersion of fine particles along with reduced crystalline fraction and an increase in the amorphous nature of KPN. Conclusion PVP K30 solid dispersions of KPN exhibited a noteworthy enhancement in the dissolution efficacy of KPN. Moreover, physical mixtures of KPN exhibited better dissolution profiles with D-mannitol and PVP K30 in comparison to pure KPN.

A Novel Endodontic Approach in Removing Smear Layer Using Nano and Submicron Diamonds with Intracanal Oscillation Irrigation.

Sodium hypochlorite (NaOCl) and ethylenediaminetetraacetic acid (EDTA) are commonly recommended for effectively removing organic and inorganic components in the smear layer. This layer is found on root canal walls after root canal instrumentation. However, high-concentration EDTA reduces the strength of dentin and the dissolution efficacy of organic substances in NaOCl solution. The objective of this study was to investigate the efficacy of applying nano and submicron diamonds in irrigation solutions with sonic and ultrasonic oscillation for removing the smear layer during endodontic treatment. Extracted single-rooted human teeth were instrumented with ProTaper® Gold (Dentsply Sirona) nickel-titanium rotary instruments. Subsequently, each canal was irrigated with 3% NaOCl, 17% EDTA, distilled water, and 10-1000 nm-sized nano and submicron diamond irrigation solutions, respectively. Sonic and ultrasonic instruments were compared for oscillating the irrigation solutions. The teeth were processed for scanning electron microscopy to observe the efficiency of smear layer removal on the canal walls. Our results indicated that diamond sizes of 50 nm and above irrigation solutions showed significant effectiveness in removing the smear layer following the oscillation of sonic instruments for 10 s. Ultrasonic assisted 500 nm and 1000 nm diamond solutions significantly differed from the other diamond-sized solution in their ability to remove the smear layer. These results suggest that sonic and ultrasonic oscillation with specific sizes of nano and submicron diamond irrigation solution can be used as an alternative approach to removing the smear layer during endodontic treatment. The potential clinical application of root canal treatments can be expected.

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Effect of two different sonic activation techniques on organic tissue dissolution efficacy of sodium hypochlorite irrigation solution: EndoActivator / Eddystrength

Effect of two different sonic activation techniques on organic tissue dissolution efficacy of sodium hypochlorite irrigation solution: EndoActivator / Eddystrength

Efavirenz dissolution enhancement V - A combined top down/bottom up approach on nanocrystals formulation

Efavirenz is one of the most commonly used drugs in HIV therapy. However the low water solubility tends to result in low bioavailability. Drug nanocrystals, should enhance the dissolution and consequently bioavailability. The aim of the present study was to obtain EFV nanocrystals prepared by an antisolvent technique and to further observe possible effect, on the resulting material, due to altering crystallization parameters. A solution containing EFV and a suitable solvent was added to an aqueous solution of particle stabilizers, under high shear agitation. Experimental conditions such as solvent/antisolvent ratio; drug load; solvent supersaturation; change of stabilizer; addition of milling step and solvents of different polarities were evaluated. Suspensions were characterized by particle size and zeta potential. After freeze- dried and the resulting powder was characterized by PXRD, infrared spectroscopy and SEM. Also dissolution profiles were obtained. Many alterations were not effective for enhancing EFV dissolution; some changes did not even produced nanosuspensions while other generated a different solid phase from the polymorph of raw material. Nevertheless reducing EFV load produced enhancement on dissolution profile. The most important modification was adding a milling step after precipitation. The resulting suspension was more uniform and the powder presented grater enhancement of dissolution efficacy.

Efficacy of medical dissolution for suspected struvite cystoliths in dogs.

BackgroundMedical dissolution of struvite uroliths in dogs is commonly recommended, but data on success rates and complications are limited.ObjectivesTo evaluate the efficacy of medical dissolution for suspected struvite cystoliths in dogs.AnimalsFifty client‐owned dogs fed a therapeutic dissolution diet, with or without administration of antimicrobials, for treatment of suspected struvite cystoliths.MethodsSingle institution, retrospective case series. Medical records were reviewed for dogs with at least 1 follow‐up visit. Dissolution success, complications, and possible predictors of success were evaluated.ResultsFull dissolution of cystoliths was achieved in 58% (29/50) of dogs within a median of 35 days (range, 13‐167). Of 21 dogs without success, 7 each had partial dissolution, no dissolution, or undetermined outcome. Uroliths containing >10% nonstruvite mineral were common in the nonsuccess group (11/16 analyzed). Maximum urolith diameter, number of uroliths, and baseline urine pH did not differ significantly between dogs with and without success. Dissolution was more likely in dogs receiving antimicrobial therapy (OR = 16.3, 95% confidence interval 1.9‐787.4, P = .002). Adverse events occurred in 9 dogs (18%); urethral obstructions were the most common, but 3 of 4 dogs with this complication were obstructed on presentation, before trial initiation.Conclusions and Clinical ImportanceResults support a medical dissolution trial for dogs with suspected struvite cystoliths. If no reduction in urolith size or number occurs by 1 month, a nonstruvite composition is likely, and alternative interventions should be considered. Dogs presenting with urethral obstructions should not be considered candidates for medical dissolution.

Urolithiasis in cats: Evaluation of trends in urolith composition and risk factors (2005-2018).

BackgroundUrolithiasis is an important upper and lower urinary tract disease in cats that results in morbidity and mortality.ObjectiveTo describe trends in composition of uroliths in cats and evaluate risk factors related to age, breed, sex, urolith location, and bacterial urolith cultures.Sample PopulationA total of 3940 uroliths and the cats from which they were obtained.MethodsThe database of the UC Davis Gerald V. Ling Urinary Stone Analysis Laboratory was searched for all urolith submissions from cats between January 2005 and December 2018. Mineral type, age, breed, sex, and urolith location and culture results were recorded. Trends were evaluated and variables compared to evaluate risk factors.ResultsA significant decrease in the proportion of calcium oxalate (CaOx)‐containing uroliths occurred over time (P = .02), from 50.1% (204/407) of all submissions in 2005 to 37.7% (58/154) in 2018. In contrast, the proportion of struvite‐containing uroliths increased significantly (P = .002), from 41.8% (170/407) in 2005 to 54.5% (84/154) in 2018. The proportion of CaOx‐containing uroliths in the upper urinary tract was significantly higher compared to the proportion of other urolith types in the upper urinary tract. Urate‐containing uroliths were the third most common type (361/3940, 9.2%). Overall, sex and age predispositions were similar to those reported previously.Conclusions and Clinical ImportanceThe decrease in the proportion of CaOx‐containing uroliths and increase in the proportion of struvite‐containing uroliths warrants investigation. Further education regarding the efficacy of medical dissolution of struvite‐containing uroliths is recommended.

ROOT CANAL IRRIGANT COMBINING SALVADORA PERSICA WITH SODIUM HYPOCHLORITE – ANTIMICROBIAL, TISSUE DISSOLUTION ,CHELATING ACTION & CHANGES IN CA/P OF ROOT DENTIN :IN VITRO STUDY

OBJECTIVE: Currently none of the irrigants used in endodontic therapy tested so far either alone or in combination could satisfy all criteria of ideal irrigant. Search for such a single agent which is more biocompatible along with other properties of irrigant continues. This study is aimed to evaluate pulp dissolution, antimicrobial activity, smear layer removing ability, and change in the Ca/P ratio of root dentin by using experimental formulation combining 3 % &amp; 5 % Sodium hypochlorite with 40% Salvadora Persica &amp; comparing it with 3 % Sodium Hypochlorite &amp; 17%EDTA Materials and Methods: Pulp dissolution: Human pulp tissue weighing 0.9g was dissolved in each experimental group G1:3%NaOCl,G2:3%NaOCl+40% S.persica, G3: 5%NaOCl +40% S.persica and weighed after the passage time of 10 min , 20min , 30 min. The difference in weight of the tissue sample before and after exposure to the test solution was assessed. Antibacterial activity: Antimicrobial efficacy of 3% NaOCl, 3% NaOCl + 40% S.Persica,5%NaOCl + 40% S.persica as experimental group against E.fecalis was assessed using direct contact test. Statistical Analysis for both the test was carried out using Kruskal Wallis and Post Hoc Mann Whitney Analysis Smear layer removal&amp; Ca/p ratio analysis: Single rooted premolars were divided in 3 groups (n=33) and irrigated with G1: 17% EDTA , 3% NaOCl, G2 : 3% NaOCl+ 40% S. persica, G3: 5% NaOCl + 40% S.persica. Each tooth was then split longitudinally. One half of sample from each group were subjected to scanning electron microscope to assess smear layer removal and second half for EDX analysis to check Ca/P ratio. Statistical Analysis: SEM – Kruskal Wallis and Post Hoc Mann Whitney EDX – ANOVA and Tukey’S HSD Post hoc Analysis RESULTS: • Pulp dissolution by freshly mixed G3 was superior to G1 &amp; G2. There is no difference in pulp dissolution efficacy of G1 &amp; G2. • No statistically significant difference was seen with respect to smear layer removal among the groups tested. EDX analysis showed significantly low Ca/P ratio for G1 compared to other groups and no statistically significant difference was seen b/w G2 &amp;G3 • In both the time interval tested (5 min, 10min) G3 showed maximum antimicrobial efficacy followed by G1 and G2 in terms of mean value. CONCLUSION: The combined formulation of 5% NaOCl + 40 % S.Persica was most effective root canal irrigant among the groups tested in terms of pulp dissolution, antimicrobial &amp;chelating action. 3% NaOCl + 40% Salvador persica was found to be as effective as 3% NaOCl and 17% EDTA. Experimental irrigants were found to be less erosive to root dentin in both combinations tested.

Efficacy and Cytotoxicity of Binary Mixtures as Root Canal Filling Solvents.

Objectives: This study reports the efficacy of two solvent mixtures on the dissolution of gutta-percha and AH Plus sealer, together with the cytotoxicity. Methods: Methyl ethyl ketone (MEK), orange oil, tetrachloroethylene, MEK/tetrachloroethylene (1:1), MEK/orange oil (1:1), and chloroform (control) were tested. Twelve groups (n = 15) of standardized stainless-steel molds filled with softened gutta-percha cones and twelve (n = 15) filled with AH Plus were immersed in the corresponding mixture or individual solvent, in an ultrasonic bath, for either 2 or 5 min. The effect of the solvents was assessed qualitatively by a topographical analysis (scanning electron microscopy) and chemical analysis (Fourier transform infrared spectroscopy), and quantitatively by a weight loss and viscoelastic property (dynamic mechanical analysis) evaluation. The cytotoxicity was assessed on MG63 human osteoblastic cells. Results: The mixtures did not show the formation of new compounds. Both presented significantly higher efficacies compared to their individual solvents, suggesting a synergistic effect. Their dissolution efficacy was similar to that of chloroform, showing high cytocompatibility. Conclusions: The proposed strategy, incorporating ultrasound agitation and profiting from the synergy of adequate solvents, might enhance root canal cleanliness allowing a single-step procedure to dissolve gutta-percha and the sealer remnants, while assuring cytocompatibility with the periapical tissues.

STATISTICAL INTERPRETATION AND OPTIMIZATION OF VALSARTAN FLOATING TABLETS USING BOX-BEHNKEN DESIGN

Objective: The main purpose of this study was to formulate and statistically evaluate 300 mg floating tablets of valsartan.&#x0D; Methods: Floating tablets of valsartan was prepared in 16 station rotary punching machine by considering 300 mg of valsartan as drug, 40-60 mg of hydroxypropyl methylcellulose (HPMC) K100M and 20-40 mg of poly (styrene-divinylbenzene) as polymers and 20 mg of sodium bicarbonate as gas generating agents. Since upper stomach has maximum therapeutic window for valsartan absorption, hence Gastroretentive Floating Tablets (GRFTs) was prepared by implementing Box-Bentham Design. The pre and post compression parameters were optimized using Statistica 10 software. From the in vitro buoyancy and drug release studies and interpretation of statistical outcomes viz. Akaike Information Criterion (AIC), Bayesian Information Criterion (BIC), Root Mean Squared Error (RMSE), Dissolution Efficiency (DE), Mean Dissolution Time (MDT), desirability study, it was concluded that batch VF5 formulation was found to be the most optimized formulation.&#x0D; Results: The floating time of VF5 was found to be 132±0.33 sec, in vitro buoyancy time was 18 h, Akaike Information Criterion (AIC) was 54.97, Bayesian Information Criterion (BIC) was 5.13, percentage dissolution efficacy was 56.39%, mean dissolution time was 5.19hr. Further, six-month stability study was performed as per ICH QIA guideline. After performing two-way ANOVA within stability study response variables, it was confirmed that the interaction was most significant.&#x0D; Conclusion: Valsartan floating drug delivery system was successfully developed by considering HPMC K100M and poly (styrene-divinylbenzene) as polymers. Among all the nine batches, VF5 was found to be the best-optimized batch.

Evaluating the discriminatory power of a dissolution assay for rosuvastatin calcium capsules: Solid-state properties and dissolution media

We propose to evaluate the dissolution properties of rosuvastatin calcium (ROSC) capsules in different media to characterize the discriminatory power of the assay method. Dissolution assays were performed in media with different pH, and including the surfactant sodium dodecyl sulfate (SDS). Several immediaterelease formulations were manufactured using the commercial raw material characterized as amorphous solid. The hydrophobic adjutant magnesium stearate was employed in some formulations due to its negative effect in the wettability and dissolution efficacy of solid dosages. These formulations showed the lower dissolution efficacy values in media without surfactant; however, when SDS was added to the medium, the dissolution efficacy increased, and the discriminatory power was lost. In spite of micellar solubilization does not increase the ROSC solubility, it modifies the discriminatory power of the assay method, increasing the wettability of the powder mixtures. The crystalline form M of ROSC was recrystallized in our laboratory, and it showed lower solubility in water than amorphous solid. However, its dissolution properties were not influenced by SDS. These results are important to develop dissolution assays for other hydrophilic drugs with increased water solubility, once that dissolution media with surfactants increase the wettability of the formulations, leading to an overrated dissolution rate.

Formulation Development and Optimization of Tramadol Hydrochloride Fast Dissolving Tablets with Natural Superdisintegrant

Tramadol is an opoid medication used to treat moderate to severe pain. The onset of pain relief begins usually within an hour of administration. In the present study an attempt has been made to develop fast dissolving tablets (FDT'S) of tramadol hcl using ocimum basilicum gum as natural superdisintegrant to improve disintegration time, dissolution efficacy and patient compliance. Tablets were prepared by direct compression method using different concentrations of superdisintegrant. The tablets prepared were evaluated for weight variation, hardness, friability, drug content, water absorption ratio, wetting time, in vitro disintegration and in vitro dissolution rate. All the FDT'S prepared disintegrated within 28seconds. Formulation of five batches(F1-F5) out of which batch F3 was found to have better results in compare to other formulations. F3 tablets disintegrate within 13+0.48 sec, wetting time was 15+0.03 sec and, water absorption ratio(%) was 34+0.24 and percent drug release was 99.12+0.11% in 30 min. Extensive swelling, porosity and wicking action of the natural material in the fast dissolving tablet formulation were found to be contributing its superdisintegrant action as comparable to synthetic superdisintegrants shown in literature.

Formulation and Evaluation of Solid Dispersion and Inclusion Complex of Poorly Aqueous Soluble Diacerein

The present study was focused on a poorly aqueous soluble drug (diacerein); basic structured anthracene molecule possesses defensive activity against osteoarthritis. The problem with the diacerein is its poor bioavailability (35%) which is due to its poor dissolution profile. The present study efforts to improve the dissolution profile using solubility enhancement techniques. The objective of the study was to improve the solubility of poorly soluble drug diacerein by solid dispersion technique and inclusion complex using the most compatible carriers and technique for the formulation. The prepared solid dispersion and inclusion complex were evaluated for physiochemical characteristics and dissolution efficacy. Thesolid dispersion and inclusion complex were formulated using kneading method with PVP K30 (screened to be the best among different carriers) and β-cyclodextrin respectively. The prepared formulations were characterized by FTIR, SEM, DSC and XRPD. The prepared solid dispersion and inclusion complex were then compressed into conventional tablets which were then coated with acid resistant polymer.